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CEP-11981

Cat. No. M3678

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CEP-11981 Structure
Synonym:

BOL 303213X

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5mg USD 200  USD200 Out of stock
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Quality Control & Documentation
Biological Activity

CEP-11981 is a potent orally active inhibitor of multiple targets (TIE-2, VEGF-R1, 2, and 3, and FGF-R1), which having essential and nonredundant roles in tumor angiogenesis and vascular maintenance. CEP-11981 demonstrated significant preclinical cytostatic anti-tumor activity against human UC xenografts in a murine model, which was attributable to inhibition of angiogenesis. Clinical development of CEP-11981 in tolerable combination regimens and the discovery of tumor and host related biomarkers predictive for benefit are warranted. Pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981 selectively binds to VEGFR and Tie2 receptor tyrosine kinases, which may result the inhibition of endothelial cell migration, proliferation and survival and the inhibition of tumor cell proliferation and tumor cell death.

Chemical Information
Molecular Weight 477.56
Formula C28H27N7O
CAS Number 856691-93-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Pili R, et al. Invest New Drugs. An open-label study to determine the maximum tolerated dose of the multitargeted tyrosine kinase inhibitor CEP-11981 in patients with advanced cancer.

[2] Hudkins RL, et al. J Med Chem. Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.

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  Catalog
Abmole Inhibitor Catalog




Keywords: CEP-11981, BOL 303213X supplier, VEGFR/PDGFR, inhibitors, activators

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